Benzoxazole Benzenesulfonamides as Allosteric Inhibitors of Fructose-1,6-bisphosphatase

Autor:	Thomas W. von Geldern, Celerino Abad-Zapatero, Melissa M. Daly, Charles W. Hutchins, Elizabeth H. Fry, Chunqiu Lai, Rebecca J. Gum
Rok vydání:	2006
Předmět:	Models Molecular Stereochemistry Clinical Biochemistry Allosteric regulation Fructose 1 6-bisphosphatase Compound 17 Pharmaceutical Science Biochemistry Chemical synthesis chemistry.chemical_compound Allosteric Regulation Pharmacokinetics Drug Discovery Hydrolase Animals Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Sulfonamides biology Organic Chemistry General Medicine Benzoxazole Combinatorial chemistry Fructose-Bisphosphatase Rats Bioavailability Enzyme chemistry Enzyme inhibitor biology.protein Molecular Medicine
Zdroj:	ChemInform. 37
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200627131
Popis:	A series of novel benzoxazole benzenesulfonamides was synthesized as inhibitors of fructose-1,6-bisphosphatase (FBPase-1). Extensive SAR studies led to a potent inhibitor, 53 , with an IC 50 of 0.57 μM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats.
Databáze:	OpenAIRE
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